Substances which act at the level of the central nervous system (CNS) are available biochemical tools for elucidating the mechanism of neurotransmission. Compounds which produce sustained tremors are also useful in simulating malfunctional and abnormal states in the CNS. A general synthetic approach is proposed for the preparation of the naturally occurring tremorgens, verruculogen and fumitremorgen. The synthetic schemes are specifically designed to provide rapid access to rationally designed structural analogues which contain the essential features for tremorgenic activity. These mycotoxins induce severe tremors in laboratory animals and are suspected of acting at the CNS by interfering with normal GABA function. This activity suggests these compounds have potential as probes for defining the role of GABA mediated neurotransmission and simulating certain neurological disorders.